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Compositions Containing Berberine or Analogs Thereof for Treating Rosacea or Red Face Related Skin Disorders

a technology of rosacea and red face, applied in the direction of drug compositions, immunological disorders, antibacterial agents, etc., can solve the problems of unfavorable treatment of rosacea by other anti-inflammatory agents and unfavorable treatment of rosacea

Active Publication Date: 2012-06-28
DERMAN BIOMEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0017]There is a need for an effective therapy for the treatment of rosacea and other related skin disorders with minimal side effects. The present invention pertains to topical pharmaceutical formulations that are effective and safe in treating rosacea and other red face related skin disorders, such as acne, seborrheic dermatitis, contact dermatitis and photodermatitis. This invention recognizes the deficiency in currently available topical pharmaceutical formulations or experimented formulations that contain berberine as a component, and improves over this deficiency.
[0046]The results of our clinical studies have shown that the topical pharmaceutical formulations of this invention containing purified berberine at concentrations higher than 0.1% or palmatine at concentrations higher than 0.02% can be efficacious, safe and well tolerable for the treatment of rosacea and red skin related disorders, such as acne, contact dermatitis, seborrheic dermatitis and photodermatitis, steroid-induced rosacealike dermatitis, and EGFR inhibitors induced acneiform dermatitis.

Problems solved by technology

While the presence of microorganisms has been examined as a potential contributing factor to rosacea, results have been inconclusive1.
However, other anti-inflammatory agents are not effective in treating rosacea.
Other traditional topical agents that have been used in a “off label” fashion include clindamycin, sulfacetamide and sulfur, but their mechanism is not well understood.

Method used

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  • Compositions Containing Berberine or Analogs Thereof for Treating Rosacea or Red Face Related Skin Disorders
  • Compositions Containing Berberine or Analogs Thereof for Treating Rosacea or Red Face Related Skin Disorders
  • Compositions Containing Berberine or Analogs Thereof for Treating Rosacea or Red Face Related Skin Disorders

Examples

Experimental program
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Effect test

example 1

Effects of Berberine on Inhibiting Cathelicdin Peptides-Induced Cytokine Secretion by Human Keratinocytes (In Vitro Assay)

[0028]For our in vitro study, berberine (Sigma, St. Louis, Mo., USA) was dissolved in water, methanol, ethanol or dimethyl sulfoxide (DMSO). Normal human keratinocytes (Invitrogen, CA, USA) were grown in EpiLife medium (Invitrogen, CA, USA) supplemented with 0.06 mM Ca+2, 1% EpiLife defined growth supplement, and 1% penicillin / streptomycin (Invitrogen, CA, USA). Cells were grown at 37° C. in a humidified atmosphere of 5% CO2 and 95% air. The human keratinocytes were cultured to confluence and treated with synthetic cathelicidin peptides (LL-37) (6.4 μM) for 16 h to induce inflammatory response similar to that observed in rosacea. Some of the cathelicidin-treated keratinocyte cultures were co-incubated with berberine of concentrations from 1.25 μg / ml to 12.5 μg / ml. The keratinocytes cultures treated with cathrlicidin or cathrlicidin with 1% ethanol and without ber...

example 2

Preparation of Topical Pharmaceutical Formulations Containing Purified Berberine and Palmatine at Defined Percentages

[0030]Based on the rationale described above, the topical berberine-containing pharmaceutical formulations of this invention have one key feature: it contains purified berberine at defined percentages that are higher than can be obtained in previous formulations using extracts of berberine-rich plants. The ranges of concentrations were subjected to tests in animal model studies and human clinical studies.

[0031]For our studies on animal models and human patients, purified berberine was dissolved in 100% ethanol, and then water was added to reach a desired concentration of berberine in the final solution. In the gel formulation, for example, 0.1% or 0.2% berberine was prepared in 10% ethanol. The solution or gel formulation were capped and stored at 4° C. until use. The results of our studies in animal models and human patients with rosacea indicate that the concentrati...

example 3

The Effects of the Topical Pharmaceutical Preparation of this Invention on a Mouse Model of Rosacea

[0035]The animal model of rosacea: the animal model of rosacea was adopted from previous reported18. Briefly, BALB / c and C57BL / 6 mice, shaved 24 h before treatments, were injected subcutaneously on the back with 40 μl of cathelicdin peptide (320 μM) twice a day. Forty-eight hours after the initial injection (four injections in total), erythema and edema were observed on the injected site mimicking the clinical features of rosacea.

[0036]In our experiments, cathelicidin-injected mice were treated with or without topical berberine twice a day to observe the effect of berberine on reducing inflammation. The results showed that mice given subcutaneous injections of cathelicidin peptides induced erythema and vascular dilatation in the skin, which resembled clinical features of rosacea after 48 h. The cathelicidin-injected mice were then divided into 2 groups, which were treated with berberin...

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Abstract

The invention pertains to topical pharmaceutical formulations of berberine and its biologically equivalent analogues, such as palmatine and coptisine, for the treatment of rosacea and other red face-related skin disorders. The topical pharmaceutical formulations of this invention contain purified berberine as the primary active drug ingredient at concentrations higher than 0.1%. The invention also pertains to methods of treating rosacea and other red face related skin disorders, such as steroid-induced rosacea-like dermatitis, comprising the administration of topical pharmaceutical formulations that contain berberine or its biologically equivalent analogues, such as palmatine.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]This application is a 35 U.S.C. 371 national stage application of International Application No. PCT / CN2010 / 000983, filed Jun. 30, 2010, which claims priority to U.S. provisional application No. 61 / 221,725, filed Jun. 30, 2009, the entire contents of which are incorporated herein by reference.BACKGROUND OF THE INVENTION1. Rosasea and its Major Symptoms[0002]Rosacea is a chronic skin disease that manifests redness and swelling, primarily on the face, especially on the central facial area. Other areas affected include the scalp, neck, ears, chest, back and the eyes. Rosacea is characterized by facial flushing, erythema, telangiectasia, and inflammatory episodes with papules and pustules and, in severe cases, rhinophyma. Comedones are notably absent'.[0003]Patients with rosacea mostly have increased sensitivity of the facial skin and dry, flaking facial dermatitis, edema of the face, and persistent granulomatous papulonodules2. According to c...

Claims

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Application Information

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IPC IPC(8): A61K31/4745A61P17/10A61P31/12A61P31/04A61P31/10A61P29/00A61P17/00A61P31/00
CPCA61K9/0014A61K45/06A61K31/4375A61P17/00A61P17/06A61P17/08A61P17/10A61P19/04A61P29/00A61P31/00A61P31/04A61P31/10A61P31/12A61P37/02A61K9/06A61K2121/00A61K47/10
Inventor HUNG, SHUEN-IUCHUNG, WEN-HUNGCHANG, TSE-WEN
Owner DERMAN BIOMEDICINE
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